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药品详细

Niflumic Acid(尼氟灭酸)

化学结构式图
中文名
尼氟灭酸
英文名
Niflumic Acid
分子式
C13H9F3N2O2
化学名
2-{[3-(trifluoromethyl)phenyl]amino}pyridine-3-carboxylic acid
分子量
Average: 282.218
Monoisotopic: 282.061612157
CAS号
4394-00-7
ATC分类
M02A 未知;M01A 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

An analgesic and anti-inflammatory agent used in the treatment of rheumatoid arthritis. [PubChem]

生产厂家
    封装厂家
    参考
    Synthesis Reference Not Available
    General Reference
    1. Criddle DN, de Moura RS, Greenwood IA, Large WA: Inhibitory action of niflumic acid on noradrenaline- and 5-hydroxytryptamine-induced pressor responses in the isolated mesenteric vascular bed of the rat. Br J Pharmacol. 1997 Mar;120(5):813-8. Pubmed
    剂型
    规格
    化合物类型
    Type small molecule
    Classes
    • Aminobenzoates
    Substructures
    • Aminobenzoates
    • Hydroxy Compounds
    • Acetates
    • Aliphatic and Aryl Amines
    • Pyridines and Derivatives
    • Halogen Derivatives
    • Benzene and Derivatives
    • Carboxylic Acids and Derivatives
    • Aminopyridines and Derivatives
    • Heterocyclic compounds
    • Aromatic compounds
    • Anilines
    适应症
    药理
    Indication Used in the treatment of rheumatoid arthritis.
    Pharmacodynamics Niflumic acid, a nonsteroidal anti-inflammatory fenamate, is a Ca2+-activated Cl- channel blocker.
    Mechanism of action Niflumic acid is able to inhibit both phospholipase A2 as well as COX-2, thereby acting as an antiinflamatory and pain reduction agent.
    Absorption Well absorbed following oral administration.
    Volume of distribution Not Available
    Protein binding 90% bound to plasma proteins.
    Metabolism
    Hepatic.
    Route of elimination Not Available
    Half life 2.5 hours
    Clearance Not Available
    Toxicity Oral, mouse: LD50 = 350 mg/kg; Oral, rat: LD50 = 250 mg/kg
    Affected organisms
    • Humans and other mammals
    Pathways Not Available
    理化性质
    Properties
    State solid
    Experimental Properties
    Property Value Source
    melting point 203 °C Not Available
    water solubility 19 mg/L (at 25 °C) YALKOWSKY,SH & DANNENFELSER,RM (1992)
    logP 4.43 TAKACS-NOVAK,K ET AL. (1995)
    Predicted Properties
    Property Value Source
    water solubility 8.83e-02 g/l ALOGPS
    logP 4.33 ALOGPS
    logP 3.12 ChemAxon
    logS -3.5 ALOGPS
    pKa (strongest acidic) 1.88 ChemAxon
    pKa (strongest basic) 5.51 ChemAxon
    physiological charge -1 ChemAxon
    hydrogen acceptor count 4 ChemAxon
    hydrogen donor count 2 ChemAxon
    polar surface area 62.22 ChemAxon
    rotatable bond count 4 ChemAxon
    refractivity 65.93 ChemAxon
    polarizability 24.21 ChemAxon
    药物相互作用
    食物相互作用
    Not Available

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